ISATIN AS A PRIVILEGED STRUCTURE IN THE DISCOVERY OF NEW ANTINEOPLASTIC MEDICINES

ISATIN AS A PRIVILEGED STRUCTURE IN THE DISCOVERY OF NEW ANTINEOPLASTIC MEDICINES

• Author
• Alejandra Marigia Fragoso dos Santos
• Co-authors
• Nathalya Patricia dos Santos soares , Allan Moraes Silva , Beatriz Silva de Arruda Cardoso , Robert da Silva Tiburcio
• Abstract

• INTRODUCTION

  The relationship between human beings and the environment is evolving in an abrasive and destructive manner, paving the way for the emergence of new multifactorial diseases, such as cancer, which requires the discovery of effective pharmacotherapeutic interventions with fewer adverse effects.1 In this context, the potential for developing new drugs using the isatin nucleus may represent a strategy in the pursuit of new lead compounds.

  AIMS

  Describe and demonstrate the relevance of the isatin nucleus in the design of new candidates for antineoplastic drugs, its primary activities reported in the literature, and its performance in the pharmaceutical industry.

  METHODS

  This research is a narrative literature review based on articles on the topic. To guide and manage the study, the following guiding question was developed: “To what extent can the Isatin nucleus contribute to the planning of new antineoplastic drugs?”.

  RESULTS AND DISCUSSION

  Isatin is a naturally occurring alkaloid widely used in the pharmaceutical industry, in which the oxindole system is one of the most exploited cores for the development of new drugs.2

  Cancer is a multifactorial and aggressive disease, thus requiring studies aimed at effective treatments with fewer adverse effects on the health and quality of life of the patient. In this way, the molecule isatin emerges as a precursor to various anticancer drug discoveries, such as Sutent® and Palladia®.3 Additionally, imatinib, erlotinib, and lapatinib are other drugs synthesized using the isatin heterocyclic scaffold as a compound, which has shown efficacy in the treatment and recovery of oncology patients health.4Hybridization is a strategy in pharmaceutical chemistry, which is one of the most effective ways to increase the molecule's activity and reduce toxic effects.

  Furthermore, the fluoroquinolone-isatin combination represents two pharmacophoric groups chemically bonded to provide not only antitumor activity but also potential antimicrobial, antitubercular, and antiviral effects.5 In this regard, a complex formed by isatin-3-ethyl-thiosemicarbazone has demonstrated significant potential as an antiproliferative agent with high cytotoxic action against cisplatin-resistant ovarian, lung, breast, and lung fibroblast cancer.6

  CONCLUSION

  In light of the above, there is a great diversity in terms of the usefulness of the heterocyclic compound isatin for the design of new drugs, as well as the optimization of existing ones, resulting in improved adherence and effectiveness in treatments

  ACKNOWLEDGMENT

  We first thank God for giving us the light of knowledge, strength, and determination to carry out this research. We also express our gratitude to Professor Mr. Robert Tibúrcio for the opportunity to guide us in this work.

  Keywords

  Isatina, Emergentes, Doenças, Planejamento, Câncer.

   

  Citations and References

  1DE CARVALHO, Jair Antonio et al. Emerging diseases: an analysis of the relationship between humans and their environment. Praxis Journal, v. 1, n. 1, 2009.

  2Czelen, Przemyslaw et al. 'Design and Synthesis of New Isatin Derivatives as Potential CDK2 Inhibitors.' International Journal of Molecular Sciences, vol. 23, no. 14, 8046. July 21, 2022, doi:10.3390/ijms23148046.

  3Dantas, L. C. (2019). Design and Synthesis of Phenylhydrazonic Derivatives of the Isatin Core.

  4Xu, Zhi et al. “Fluoroquinolone-isatin hybrids and their biological activities.” European journal of medicinal chemistry vol. 162 (2019): 396-406. doi:10.1016/j.ejmech.2018.11.032

  5ROSAS, Monica SL et al. Cancer incidence in Brazil and the potential use of isatin derivatives in experimental oncology. Virtual Journal of Chemistry, v. 5, n. 2, p. 243-265, 2013.

  6LIMA, Andresa Alves de. Synthesis, evaluation of antiproliferative activity, and study of interaction with DNA of a silver compound containing isatin-derived thiosemicarbazone. 2022.

   

   

• Keywords
• Isatin, Emerging, Diseases, Planning, Cancer.
• Modality
• Pôster
• Subject Area
• Drug Design and Discovery, Synthesis and Natural Products